DP Antagonist

Laropiprant is a potent and selective DP receptor antagonist with K_i values of 0.57 nM and 2.95 nM for DP receptor and TP Receptor, respectively.

Asapiprant is a potent and selective DP₁ receptor antagonist with a K_i of 0.44 nM.

AGN 225660 is a multi-prostanoid receptor antagonist with human IC₅₀ values of 70, 70, 5, 220 and 180 nM for EP1, EP4, TP, DP1, FP. AGN 225660 inhibits secretion of RANTES, IL-8, MCP-1, IL-12p70, and IL-23. AGN 225660 exhibits good ocular bioavailability and reduces ocular inflammation linked to phacoemulsification surgery and uveitis.

AZ-11665362 is a CRTh2 (DP2) receptor antagonist with an IC₅₀ of 2.6 nM. AZ-11665362 shows weak activity against aldose reductase, serotonin transporter, CYP 2C19, and CYP 2C9. AZ-11665362 lacks measurable inhibitory activity against COX-1 and COX-2. AZ-11665362 can be used for the research of asthma, and other inflammatory diseases.

Fevipiprant (QAW039, NVP-QAW039) is s an orally active, selective, reversible prostaglandin D2 (DP2) receptor antagonist with an K_d value of 1.14 nM. Fevipiprant has the potential for the research of bronchial asthma.

Timapiprant (OC000459) is a potent, selective, and orally active D prostanoid receptor 2 (DP₂, also known as CRTH2) antagonist. Timapiprant (OC000459) potently displaces [³H] PGD2 from human recombinant DP₂ (K_i=13 nM), rat recombinant DP₂ (K_i=3 nM), and human native DP₂ (K_i=4 nM). Timapiprant (OC000459) inhibits mast cell activation of Th2 lymphocytes and eosinophils.

Ramatroban is a selective thromboxane A₂ (TxA₂, IC₅₀=14 nM) antagonist, which also antagonizes CRTH2 (IC₅₀=113 nM) by inhibiting PGD₂ binding.

AZD1981 is the antagonist for GPR44 (also known also PTGDR2, DP2 or CRTh). AZD1981 blocks the binding of PGD2 to CRTH2. AZD1981 exhibits immunomodulatory effects and can be used in research of chronic spontaneous urticaria.

BW A868C, a hydantoin compound, is a BW245C structural analogue. BW A868C is a selective and potent competitive prostaglandin D2 (PGD2) antagonist. BW A868C has no effect on other prostaglandin receptors (IP, EP1, EP2, TP and FP).

CAY10471 (TM30089) is a potent, selective, and orally active prostaglandin D2 receptor CRTH2 antagonist. CAY10471 attenuates the progression of tubulointerstitial fibrosis and chronic contact hypersensitivity (CHS) in animal model.

BI-671800 is a highly specific and potent antagonist of chemoattractant receptor-homologous molecule on Th2 cells (DP2/CRTH2), with IC₅₀ values of 4.5 nM and 3.7 nM for PGD2 binding to CRTH2 in hCRTH2 and mCRTH2 transfected cells, respectively. BI-671800 has potential for the treatment of poorly controlled asthma.

L 888607 Racemate is a selective prostaglandin D₂ receptor subtype 1 (DP1) antagonist, with K_is of 132 nM and 17 nM for DP1 and thromboxane A2 receptor (TP), respectively.

Setipiprant (ACT-129968) is an orally active and selective CRTH2 antagonist. Setipiprant interacts with hCRTH2 receptor with an IC₅₀ value of 6 nM. Setipiprant inhibits prostanoid receptors hDP₁ and hEP₂ with IC₅₀ values of 1290 and 2600 nM, respectively. Setipiprant can be used for the research of asthma and rhinitis.

CAY10471 Racemate (TM30089 Racemate) is a potent and highly selective prostaglandin D2 receptor CRTH2 antagonist, with a K_i of 0.6 nM for hCRTH2, selective over human thromboxane A2 receptor TP (K_i, >10000 nM) or PGD2 receptor DP (K_i, 1200 nM). CAY10471 Racemate also has effect on mouse and rat orthologs of CRTH2.

MK-7246 is a potent and selective CRTH2 antagonist with a K_i of 2.5±0.5 nM.

Pexopiprant is an oral antagonist of the prostaglandin D2 receptor 2 (DP2),K_i ＜ 100nM. Pexopiprant can be used in studies of asthma.

AMG-009 is a potent antagonist of prostaglandin D2, with IC₅₀ of 3 nM and 12 nM for CRTH2 and DP receptors, respectively.

Laropiprant sodium is a potent and selective DP receptor antagonist with K_i values of 0.57 nM and 2.95 nM for DP receptor and TP Receptor, respectively.

MK-8318 is a potent and selective CRTh2 receptor antagonist with a K_i of 5.0 nM.

AM-461 is a DP2 receptor (Prostaglandin Receptor) antagonist. AM-461 can be used for the researches of inflammation and immunology, such as asthma.